Category: Glioblastoma

AMG-458 is a Selective and Orally Bioavailable c-Met Inhibitor

C-met is a protein encoded by a met gene in humans, which has tyrosine kinase activity. Specifically, Met is an essential one-way tyrosine kinase receptor for embryonic development, organogenesis, and wound healing. Besides, C-met is a receptor tyrosine kinase that can be activated by its ligand, hepatocyte growth factor/dispersion...

TED-347 is an Irreversible and Covalent YAP-TEAD Protein-Protein Interaction Inhibitor

Yap1, also known as Yap, is a protein that acts as a transcription regulator by activating the transcription of genes involved in cell proliferation and inhibiting apoptosis. Specifically, Yap1 is inhibited in the hippopotamus signaling pathway, which can control organ size and inhibit tumors. Besides, hippopotamus signaling regulates Yap1...

AMG 511 is an Orally Active pan-PI3K Inhibitor

The PI3K signaling network has a central role in several cellular processes critical to the initiation and progression of cancer, including growth, survival, and metabolism. The PI3K family catalyzes the phosphorylation of phosphatidylinositol-4,5-diphosphate to phosphatidylinositol-3,4,5-triphosphate, a secondary messenger that plays a critical role in important cellular functions such as...

Gboxin is an Oxidative Phosphorylation Inhibitor That Targets Glioblastoma

According to the World Health Organization (WHO), Glioblastoma is the most common primary brain neoplasm. It comprises 15% of all intracranial neoplasms and 60-75% of astrocytic tumors. Unfortunately, Glioblastoma is the most aggressive and prevalent primary malignant brain tumor of the central nervous system. Glioblastoma derives specifically from the...

RIPGBM is a Selective Inducer of Apoptosis in Glioblastoma Multiforme Cancer Stem Cells

Glioblastoma multiforme is the most prevalent and aggressive form of primary brain cancer. Glioblastoma multiforme is the most hostile type of brain cancer. Its aggressiveness is due to increased invasion, migration, proliferation, angiogenesis, and a decreased apoptosis. Crucially, a sub-population of multi-potent cells term glioblastoma multiforme cancer stem cells...

JR-AB2-011, a Potential Inhibitor of mTORC2 Activity in Glioblastoma Multiforme (GBM)

Glioblastoma multiforme (GBM) are highly malignant and invasive tumors. It not only can prevent total surgical resection, but also render these neoplasms refractory to cheJR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM). JR-AB2-011...